WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 555128
CAS#: 1414797-35-5
Description: GSK2973980A is a potent and selective DGAT1 inhibitor (hDGAT1 LE IC50 = 3 nM). GSK2973980A demonstrates excellent DMPK profiles and in vivo efficacy in a postprandial lipid excursion model in mice. Based on the overall biological and developability profiles and acceptable safety profiles in the 7-day toxicity studies in rats and dogs, GSK2973980A was selected as a candidate compound for further development in the treatment of metabolic disorders.
MedKoo Cat#: 555128
Name: GSK2973980A
CAS#: 1414797-35-5
Chemical Formula: C25H19F5N4O4
Exact Mass: 534.1326
Molecular Weight: 34.443
Elemental Analysis: C, 56.18; H, 3.58; F, 17.77; N, 10.48; O, 11.97
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Synonym: GSK2973980A; GSK-2973980A; GSK 2973980A;
IUPAC/Chemical Name: (S)-2-(6-(5-(3-(3,4-difluorophenyl)ureido)pyrazin-2-yl)-1-oxo-2-(2,2,2-trifluoroethyl)-1,2,3,4-tetrahydronaphthalen-2-yl)acetic acid
InChi Key: OTKTZEZTFCAULO-DEOSSOPVSA-N
InChi Code: InChI=1S/C25H19F5N4O4/c26-17-4-2-15(8-18(17)27)33-23(38)34-20-11-31-19(10-32-20)14-1-3-16-13(7-14)5-6-24(22(16)37,9-21(35)36)12-25(28,29)30/h1-4,7-8,10-11H,5-6,9,12H2,(H,35,36)(H2,32,33,34,38)/t24-/m0/s1
SMILES Code: O=C(O)C[C@@](CCC1=C2C=CC(C3=NC=C(NC(NC4=CC=C(F)C(F)=C4)=O)N=C3)=C1)(CC(F)(F)F)C2=O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 34.443 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Discovery of Tetralones as Potent and Selective Inhibitors of Acyl-CoA:Diacylglycerol Acyltransferase 1
Mui Cheung, Raghuram S. Tangirala, Sridhar R. Bethi, Hemant V. Joshi, Jennifer L. Ariazi, Vijaya G. Tirunagaru, and Sanjay Kumar
Publication Date (Web): January 16, 2018 (Letter)
DOI: 10.1021/acsmedchemlett.7b00450
Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) plays an important role in triglyceride synthesis and is a target of interest for the treatment of metabolic disorders
